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Design of a multivalent bifunctional chelator for diagnostic <sup>64</sup> Cu PET imaging in Alzheimer’s disease

Hong-Jun Cho, Truc T. Huynh, Buck E. Rogers, Liviu M. Mirica

2020Proceedings of the National Academy of Sciences40 citationsDOIOpen Access PDF

Abstract

Significance Metal radiotracers exhibit beneficial properties that can improve in vivo positron emission tomography (PET) imaging over traditional radionuclides, such as longer half-lives, facile last-stage radiolabeling steps, and the potential for dual imaging-therapy applications. Among such radionuclides, 64 Cu exhibits a longer half-life (t 1/2 = 12.7 h) that allows for later PET imaging times and the ability to distribute 64 Cu imaging agents to facilities that do not have an on-site cyclotron. Herein, we report a 64 Cu PET imaging agent that shows appreciable in vivo brain uptake and exhibits high specific affinity for beta-amyloid aggregates, leading to the successful PET imaging of amyloid plaques in the brains of 5xFAD mice versus those of wild-type mice.

Topics & Concepts

Positron emission tomographyPet imagingIn vivoPreclinical imagingImaging agentRadiochemistryNuclear medicineMolecular imagingAmyloid (mycology)ChemistryNeuroimagingChelationMedicinePathologyBiologyBiotechnologyPsychiatryOrganic chemistryMedical Imaging Techniques and ApplicationsRadiopharmaceutical Chemistry and ApplicationsLanthanide and Transition Metal Complexes
Design of a multivalent bifunctional chelator for diagnostic <sup>64</sup> Cu PET imaging in Alzheimer’s disease | Litcius